托伐普坦片在中国健康人体的生物等效性研究

目的: 评价试验制剂托伐普坦片与参比制剂托伐普坦片在中国健康人体中的生物等效性。方法: 采用双周期随机交叉试验设计,入选24名男性健康受试者单次口服参比制剂和试验制剂 30 mg,采用高效液相色谱-串联质谱法(HPLC-MS/MS)测定血浆中托伐普坦的浓度,经DAS 2.1 软件处理参数,并进行双单侧t检验确定是否等效。结果: 试验制剂和参比制剂的主要药代动力学参数分别为:C_max为(179±97)和(189±86) μg/L;t_max为(2.5±1.1)和(2.5±1.0) h;AUC_0-t为(1153±488)和(1225±528) μg·h·L^-1;AUC_0-∞为(1161±492)和(1232±528) μg·h·L^-1;t_1/2为(5.6±2.0)和(5.6±2.0) h。试验制剂对参比制剂的相对生物利用度F为(95.8±18.7)%。结论: 试验制剂托伐普坦片与参比制剂托伐普坦片生物等效。

Bioequivalence of Tolvaptan tablets in healthy Chinese volunteers

AIM: To evaluate the bioequivalence of Tolvaptan tablets in healthy Chinese volunteers.METHODS: A single oral doses of 30 mg Tolvaptan tablets (test and reference) were given to 24 healthy volunteers according to an open randomized crossover design. The concentrations of Tolvaptan in plasma were determined by HPLC-MS/MS. The pharmacokinetic parameters of the test and reference preparation were calculated by DAS 2.1. The bioequivalence was evaluated by two one-sided t test.RESULTS: The pharmacokinetic parameters of the test and reference preparations were as follows: C_max were (179±97) and (189±86) μg/L; t_max were (2.5±1.1) and (2.5±1.0) h;AUC_0-t were (1153±488) and (1225±528) μg·h·L^-1;AUC_0-∞ were (1161±492) and (1232±528) μg·h·L^-1;t_1/2 were (5.6±2.0) and (5.6±2.0) h. The relative bioavailability of the test preparation was (95.8±18.7)%.CONCLUSION: The tested preparation was of bioequivalence to the reference preparation.